Resistance to macrolide-lincosamide-streptogramin B antibiotics is induced by 16 membered-ring macrolide antibiotics in Enterococcus faecalis 373.
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Anti-Bacterial Agents↗
Biomedical subjects
B K Kim
Publications and source records attributed to B K Kim.
Increased contractility of rat uterine smooth muscle at the end of pregnancy.
Upon stimulation with high K+, oxytocin, prostaglandin E2, prostaglandin F2 alpha or carbachol, myometrium isolated from pregnant rats (21 days after pregnancy) developed 2-3 times greater isometric force than that from non-pregnant rats (estrus). High K+ increased the level of myosin light chain (MLC) phosphorylation to a similar extent in these tissues, and therefore pregnant myometrium developed greater contraction than non-pregnant myometrium at a given MLC phosphorylation. In the permeabilized muscle with alpha-toxin, Ca2+ (0.1-10 microM) induced greater contraction in pregnant myometrium than in non-pregnant myometrium. Ca2+ sensitivity was not altered after pregnancy. MLC kinase and phosphatase activities did not differ significantly between pregnant and non-pregnant myometria. Stimulation with 10 microM Ca2+ and 1 microM calyculin-A elicited similar magnitudes of contractions in the permeabilized muscles isolated from non-pregnant and pregnant rats. SDS-PAGE showed that the percentage of the content of MLC was not altered between these preparations, although actin content increased after pregnancy. These results suggest that the stress generating capacity of myometrium is increased after pregnancy without changing the MLC phosphorylation step. The equal capacity of force generation after the maximum phosphorylation by Ca2+ and phosphatase inhibitor suggests that a MLC phosphorylation-independent mechanism is responsible for the development of greater force in the pregnant myometrium.
Actins↗
Telomerase activity in acute myelogenous leukaemia: clinical and biological implications.
We examined telomerase activity in myeloid leukaemic cell lines, normal haemopoietic cells, and leukaemic blasts from acute myelogenous leukaemia (AML) patients. Normal bone marrow mononuclear (BMNC) cells expressed low telomerase activity. Higher telomerase activity was detected in 10 myeloid leukaemic cell lines compared to normal BMNC cells. Treatment with 1,25(OH)2D3, and vitamin D3 analogues, EB1089 and KH1060, reduced telomerase activity in vitamin D3-sensitive HL-60 cells, whereas vitamin D3 insensitive K562 cells did not change its activity. This down-regulation of telomerase activity by EB1089 was associated with induction of p21 protein. The rank order of telomerase activity was leukaemic CD34- cells > leukaemic CD34+ cells > normal CD34- cells > normal CD34+ cells. Telomerase activity was positive in all of the AML patients tested; however, heterogeneity of telomerase activity was found amongst this group. Therefore we compared telomerase activity with clinical response. Unexpectedly, we found that a higher rate of complete remission was noted in AML patients with higher telomerase activity. No association between telomerase activity and biological parameters including percentage of S-phase, cytotoxicity to cytosine arabinoside and percentage of CD34+ cells in AML blasts was found. These results suggest that telomerase activity in AML patients is detected with high frequency, but is heterogenous. Expression level of telomerase activity may have a clinical implication in AML patients regarding clinical response.
Adult↗
In-vitro and in-vivo antibacterial activity of CFC-222, a new fluoroquinolone.
CFC-222 is a novel fluoroquinolone with potent and broad-spectrum antibacterial activity. The in-vitro and in-vivo activities of CFC-222 were compared with those of ciprofloxacin, ofloxacin, lomefloxacin and sparfloxacin. Against gram-positive bacteria such as Staphylococcus aureus (quinolone-susceptible and quinolone-resistant), Staphylococcus epidermidis, Streptococcus pneumoniae and Enterococcus faecalis, CFC-222 was more active than ciprofloxacin and similar to sparfloxacin. Against gram-negative bacteria, including Enterobacteriaceae, the in-vitro activity of CFC-222 was similar to that of sparfloxacin, but less than that of ciprofloxacin. However, it was less active than ciprofloxacin and sparfloxacin against Pseudomonas aeruginosa. In mouse systemic infection caused by S. aureus Smith or S. aureus TMS 33, CFC-222 demonstrated an activity similar to that of ciprofloxacin and sparfloxacin, but better than that of ofloxacin. The compound was more effective than ciprofloxacin and sparfloxacin in murine infection caused by Streptococcus pyogenes ATCC 8668. Against Escherichia coli, Klebsiella pneumoniae and Enterobacter cloacae infections, the efficacy of CFC-222 was similar to those of ciprofloxacin, ofloxacin and sparfloxacin. The activity of CFC-222 was similar to those of ciprofloxacin and sparfloxacin against P. aeruginosa MB4-16 in the same infection model. These results suggest that CFC-222 may be a promising therapeutic agent for the treatment of various bacterial infections.
Animals↗
Susceptibility of penicillin-susceptible and -resistant pneumococci to CFC-222, a new fluoroquinolone.
The in-vitro activity of 12 antibacterial agents against 98 clinical isolates of Streptococcus pneumoniae, including 54 penicillin-resistant strains, was determined by a standardized broth microdilution method. CFC-222, vancomycin and imipenem were the most active agents, with an MIC90 of 0.5 mg/L for the test strains. CFC-222 was 16-fold more potent than ciprofloxacin and ofloxacin against all strains tested, including both penicillin-susceptible and -resistant strains. The anti-pneumococcal activity of fluoroquinolones was not affected by penicillin susceptibility. These results indicate that CFC-222 is potentially useful for treating infection caused by penicillin-resistant strains of S. pneumoniae.
Anti-Infective Agents↗
The effectiveness of modified ingram therapy compared with severity of psoriasis.
To treat cases of psoriasis, various modifications of the original Ingram method were tested for increased effectiveness and minimized side reactions. Our modified method consists of 0.1-0.5% anthralin ointment application and selective UVB phototherapy with adjunctive warm water bath and the application of emollients. The object of this study was to evaluate the effectiveness and duration of remission in response to our modified Ingram method and compare the data with the severity of psoriasis. The clearing rate was higher and the failure rate was lower in the moderate group. The number of occasions on which therapy was used and the duration of this therapy were greater in the severe group, but there were no significant differences except for the number of occasions of therapy to the trunk. Fifty-eight percent of the moderate group did not relapse in more than one year, but 63% of the severe group relapsed within six months. The results of this study showed that the modified Ingram regimen is an effective therapeutic modality in psoriasis, especially in the moderate group.
Administration, Topical↗
Immunotactoid glomerulopathy associated with idiopathic hypereosinophilic syndrome.
A case of immunotactoid glomerulopathy in an 18-year-old man with an idiopathic hypereosinophilic syndrome is presented. The patient showed cervical lymphadenopathy, asymptomatic proteinuria of nephrotic range, and hematuria without any defined immunologic disease. Marked and prolonged hypereosinophilia was found in peripheral blood (eosinophil count; 6,248/mm3) and bone marrow (eosinophil series; 32%). Diffuse and/or nodular eosinophilic infiltration was identified in multiple organs such as kidney, stomach, liver, lymph node, and skin. Renal biopsy revealed endocapillary proliferative features of typical immunotactoid glomerulopathy with IgG and C3 deposition and microtubular structures of variable size, 20-80 nm in diameter, mainly in the subendothelium. This study suggests that immunotactoid glomerulopathy may be a secondary immunologic manifestation of the tissue damage by eosinophils in the idiopathic hypereosinophilic syndrome.
Adolescent↗
Alterations of p16INK4A and p15INK4B genes in gastric carcinomas.
BACKGROUND: It has been suggested that cyclin-dependent kinase inhibitors (CDKIs), including p16 and p15, are tumor suppressor genes. Alterations of CDKIs have been found in most types of cancer. However, little is known about the status of p16 and p15 genes, including methylation of the promoter region, in gastric carcinoma. METHODS: Thirty-six primary gastric tumors and 9 gastric carcinoma cell lines were examined for alterations of the p16 and p15 genes. Deletion of the p16 and p15 genes was assessed by Southern blot analysis, expression by Northern blot analysis, and mutation by polymerase chain reaction-single strand conformation polymorphism followed by direct sequencing. The methylation status of the 5' CpG island of the p16 gene was evaluated using methylation-sensitive restriction enzymes, and reversal of the transcriptional block of the p16 gene was determined by Northern blot analysis after treatment with 5-aza-2'-deoxycytidine. RESULTS: Homozygous deletions of the p16 and 15 genes from 2 of 9 gastric carcinoma cell lines were found. In contrast, no deletions were detected in 36 primary gastric tumors, and one primary tumor showed rearrangements of the p16 and p15 genes. Two gastric carcinoma cell lines showed a point mutation and an insertional mutation of the p16 gene, respectively; however, no point mutations were noted for the p16 and p15 genes in any of the primary gastric tumors. Constitutive levels of p16 mRNA expression in gastric carcinoma cell lines were quite heterogeneous; four gastric carcinoma cell lines had no detectable p16 mRNA and 6 gastric carcinoma cell lines had negligible expression of p15 mRNA. Of 10 primary gastric tumors, only 1 tumor expressed p16 mRNA. Furthermore, abnormal DNA methylation patterns of the p16 gene were found in 2 gastric carcinoma cell lines through the use of methylation-sensitive restriction enzymes. These cell lines lacked expression of p16 mRNA without deletions of the p16 gene. These transcriptional blocks were reversed by treatment with 5-aza-2'-deoxycytidine. CONCLUSIONS: Deletions or mutations of the p16 and p15 genes are uncommon in primary gastric carcinomas. However, defective mRNA transcription, sometimes by aberrant DNA methylation, might be one of the pathways of inactivation of the p16 gene that leads to the development of gastric carcinoma.
Adenocarcinoma↗
P1,P4-dithio-P2,P3-monochloromethylene diadenosine 5',5'''-P1,P4-tetraphosphate: a novel antiplatelet agent.
We have previously demonstrated in a series of searches for antithrombotic agents that diadenosine 5',5"'-P1,P4-tetraphosphate (AppppA) and its analogues are competitive inhibitors of ADP-induced platelet aggregation. Among various analogues, the P2,P3-monochloromethylene analog of AppppA (AppCHClppA) is superior to unmodified AppppA in its antiplatelet and antithrombotic effects. In this communication, we compare the antiplatelet potency of five newly synthesized agents with that of AppCHClppA. The five new agents include four diadenosine polyphosphate analogues [Ap(s)pCHClpp(s)A (p(s) indicates a thiophosphate), dAppCHClppdA, dAp,pCHClpp(s)dA, and AppCHClpCHClppA], and an adenosine tetraphosphate analogue (AppCHClpCHClp). When tested for their inhibitory effects on platelet aggregation by ADP, the most promising agent among them was Ap(s)pCHClpp(s)A. Both molecular and functional integrity of this compound proved to be stable in blood at 37 degrees C for at least 3 h. It also showed an excellent heat stability. This agent inhibits a number of aspects of ADP-induced platelet activation-e.g., release reaction, cytoplasmic calcium mobilization, thromboxane production, fibrinogen binding sites, and platelet factor 3 activity. Moreover, platelet aggregation induced by agonists other than ADP-e.g., arachidonic acid, collagen, and epinephrine-was inhibited partially by Ap(s)pCHClpp(s)A. It is concluded that (i) Ap(s)pCHClpp(s)A is a promising antiplatelet agent; (ii) it is resistant to blood phosphodiesterases and stable to heat treatment; (iii) platelet aggregation induced by collagen, epinephrine, or arachidonic acid is also inhibited in part by this agent; and (iv) specificity of the inhibitory effects is presented by unmodified adenosine moieties of the agent. Resistance to phosphodiesterases raises the possibility of oral administration.
Blood Platelets↗
Suppressive effects of Ganoderma lucidum on proliferation of peripheral blood mononuclear cells.
The basidiocarps of Ganoderma lucidum have been used for prevention and treatment of various diseases in the Orient. Methanolic extracts of this mushroom were applied to human peripheral blood mononuclear cell (PBMC) culture systems in the presence of various immunostimulating or immunosuppressive agents. Phytohemagglutinin-induced cell proliferation was reduced to 14% of that of the control by a GLE fraction that is the neutral component of the methanolic extracts of the carpophores. 12-O-tetradecanoylphorbol 13-acetate (TPA)-induced cell proliferation was inhibited by the fractions of GLA, GLC, GLE and GLG. However none of these fractions inhibited proliferation of the PBMCs stimulated with TPA plus ionomycin (IM). Treatment of the PBMCs with cyclosporin A (CsA) led to blockage of the cell proliferation to 9% of that of the control. When the cells were cultured with the methanolic fractions in the presence of CsA, concentration dependent inhibition of the cell proliferation was observed by the addition of GLE and GLG fractions. On the contrary, the GLH fraction recovered the CsA induced inhibition of the cell proliferation. Taken together, among the methanolic fractions, GLE showed the highest inhibitory activity. This fraction might inhibit the protein kinase C signal pathway and accelerate the CsA signal pathway.
Basidiomycota↗
In vitro and in vivo antibacterial efficacies of CFC-222, a new fluoroquinolone.
CFC-222 is a novel fluoroquinolone containing a C-7 bicyclic amine moiety with potent antibacterial activities against gram-positive, gram-negative, and anaerobic organisms. We compared the in vitro and in vivo activities of CFC-222 with those of ciprofloxacin, ofloxacin, and lomefloxacin. CFC-222 was more active than the other fluoroquinolones tested against gram-positive bacteria. CFC-222 was particularly active against Streptococcus pneumoniae (MIC at which 90% of isolates are inhibited [MIC90], 0.2 microg/ml), Staphylococcus aureus (MIC90, 0.2 microg/ml for ciprofloxacin-susceptible strains), and Enterococcus faecalis (MIC90, 0.39 microg/ml). Against Escherichia coli and other members of the family Enterobacteriaceae, CFC-222 was slightly less active than ciprofloxacin (MIC90s for E. coli, 0.1 and 0.025 microg/ml, respectively). The in vitro activity of CFC-222 was not influenced by inoculum size, medium composition, or the presence of horse serum. However, its activity was decreased significantly by a change in the pH of the medium from 7.0 to 6.0, as was the case for the other quinolones tested. The in vivo protective efficacy of CFC-222 by oral administration was greater than those of the other quinolones tested in a mouse model of intraperitoneally inoculated systemic infection caused by S. aureus. CFC-222 exhibited efficacy comparable to that of ciprofloxacin in the same model of infection caused by gram-negative organisms, such as E. coli and Klebsiella pneumoniae. In this infection model, CFC-222 was slightly less active than ciprofloxacin against Pseudomonas aeruginosa. These results suggest that CFC-222 may be a promising therapeutic agent in various bacterial infections.
Animals↗
Inhibition of cellular proliferation by cyclosporin A during compensatory renal growth: flow cytometric analysis.
Cell cycle analysis using flow cytometer (FCMX) was performed to evaluate the influence of cyclosporin A (CsA) on cellular proliferation during compensatory renal growth (CRG) in uninephrectomized (Ux) rats. CsA (50 mg/kg/day) was administered subcutaneously for 7 days and animals were scarificed 0, 12, 24, 48, 72, 120 and 168 h after Ux. The percent changes in the S (DNA synthesis) and G2M (DNA replication) phases in the contralateral kidney were analyzed. The cortical cells entering the S and G2M phases showed significant differences between CsA and vehicle groups (p = 0.0001, p = 0.001, respectively), but the medullary cells entering the S and G2M phases showed no significant differences between the 2 groups (p = 1.000, respectively). In the cortex, the CsA group showed a significant decrease in the S (at 12, 72 and 120 h) and G2M phases (at 24, 72 and 120 h) compared to the vehicle group (p < 0.05, respectively), but there was no significant difference in the medulla. In conclusion, cellular proliferation is suppressed in cortical cells by CsA.
Animals↗
Purely epithelioid malignant peripheral nerve sheath tumor of the vulva.
Primary malignant peripheral nerve sheath tumors(MPNST) of the vulva are extremely rare and most of them are composed of a spindle cell component. A few cases of MPNST containing partially or purely epithelioid cells have been reported. Purely epithelioid MPNST differ from the ordinary epithelioid MPNST due to the absence of a spindle cell component. We present the first case of purely epithelioid MPNST arising in the vulva reviewing in the world literature without definite evidence of von Recklinghausen's disease or nerve involvement. The patient was a 63-year-old woman with a palpable vulvar mass, 6 x 4 x 1.5 cm in dimension, was not encapsulated but well-demarcated, ovoid and rubbery and showed pale yellow, homogeneous, fish-flesh appearance with focal cystic changes on cut surface. The histologic features consisted of solely epithelioid cells which were arranged in tight clusters or cords with solid growing pattern and focally scattered rosette-like structures. According to the immunohistochemical results, most of tumor cells were strongly positive for neuron specific enolase, and some of them were weakly positive for S-100 protein and vimentin. We considered that purely epithelioid MPNST would represent a certain degree of differentiation toward nerve or neuronal cells rather than Schwann cells.
Epithelioid Cells↗
Neutrophilic dermatoses associated with myeloid malignancy.
The neutrophilic dermatoses are significantly associated with myeloid malignancies. We now describe the clinical and histological features of 11 patients with these disorders, namely Sweet's syndrome in three cases, pyoderma gangrenosum in two, and neutrophilic eccrine hidradenitis in one; there were also five others which could not be categorised as recognised entities. Our observations, as well as those from a review of the literature, support the hypothesis that in the neutrophilic dermatoses associated with myeloid malignancy, a common mechanism may be involved.
Adult↗
Protective effect of taurine on indomethacin-induced gastric mucosal injury.
It has been suggested that oxygen-derived free radicals play an important role in the pathophysiology of acute gastric ulceration induced by NSAIDs and ischemia-reperfusion. Taurine is hypothesized to exert its protective effect on NSAIDs-induced gastric injury by its antioxidant properties. The protective effect of taurine on indomethacin-induced gastric mucosal lesion and its protective mechanism were investigated. Intragastric administration of 25 mg/kg of indomethacin induced hemorrhagic lesions on the glandular stomach in rats. Pretreatment with 0.25 or 0.5 g/kg of taurine one day before or for 3 days significantly reduced gastric lesion formation and inhibited the elevation of lipid peroxide level in gastric mucosa. Both resting and FMLP-induced luminol-dependent chemiluminescence of rat peritoneal neutrophils increased immediately after treatment with indomethacin. Taurine (5-20 mM) inhibited chemiluminescence of neutrophils activated by FMLP. Human neutrophils (polymorphonuclear leukocytes) adhered to the confluent monolayer of human umbilical vein endothelial cells (HUVEC) after coincubation with indomethacin. This neutrophil adhesion induced by indomethacin to HUVEC was prevented by taurine in a dose-dependent manner. These results indicate that the protective effect of taurine against NSAIDs-induced gastric mucosal injury is due to its antioxidant effect, which inhibits lipid peroxidation and neutrophil activation.
Adult↗
Dexamethasone recovers phorbol-ester induced reduction of taurine transportation in mouse macrophage cell line, RAW 264.7.
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Animals↗
Three-year clinical follow-up after Palmaz-Schatz stenting.
OBJECTIVES: Our goals were to examine late clinical outcome in a cohort of patients who electively received Palmaz-Schatz intracoronary stents, to identify specific predictors of outcome and to determine the time course of the development of ischemic cardiac events after stenting. BACKGROUND: Short-term results of Palmaz-Schatz intracoronary stenting have been promising, with a reduction in both angiographic restenosis and clinical cardiac events up to 1 year after stenting. METHODS: We analyzed the clinical outcomes in 65 consecutive patients who underwent stenting at least 3 years before analysis. Demographic, clinical and procedural predictors of survival and event-free survival, defined as freedom from myocardial infarction, stent-site percutaneous transluminal coronary angioplasty, coronary artery bypass graft surgery or death, were analyzed at a mean follow-up of 39 +/- 17 months. RESULTS: Absolute survival and event-free survival at 3 years were 88% and 56%, respectively. Three-year freedom from stent-site revascularization was 66%. Predictors of decreased long-term survival (p < 0.05) included diabetes and a high angina score (Canadian Cardiovascular Society class III/IV) at 6 and 12 months after stenting. Predictors of decreased event-free survival (p < 0.05) included a high angina score at 3, 6 and 12 months after stenting, smaller stent deployment balloon size and greater number of stents implanted. Freedom from adverse events by 6 months after stenting also correlated with long-term event-free survival. Eighty-five percent of stent-site revascularizations occurred within 1 year. During late follow-up (>24 months), no patients had stent-site stenoses requiring revascularization, whereas 11% of patients required revascularization in nonstented coronary segments. CONCLUSIONS: Clinical predictors of worse long-term outcome included diabetes mellitus, higher angina score at follow-up, smaller stent deployment balloon size and greater number of stents at implantation. During follow-up, the majority of adverse events and stent-site revascularizations occurred early after stenting, and disease progression in nonstented vessels accounted for the majority of late revascularization events.
Aged↗
Chromosomal numerical aberrations in gastric carcinoma: analysis of eighteen cases using in situ hybridization.
Paraffin-embedded tumor cells of 18 cases of gastric carcinoma were hybridized with digoxigenin-labeled repetitive DNA probes specific for the centromeric regions of chromosomes X, Y, 1, 2, 3, 4, 6, 7, 8, 9, 10, 11, 12, 15, 16, 17, 18, and 20. All cases demonstrated numerical chromosomal aberrations. The most exciting aberration, polysomy (five or more copies) of several chromosomes, was found in all cases except a case of mucinous adenocarcinoma, which showed trisomy 9 as the sole chromosomal numerical aberration. In nine cases of tubular adenocarcinoma, poorly-differentiated polysomies of several chromosomes were the consistent numerical aberration and monosomy 7, 18(2 cases each), 10, and 17(1 case each) were also found. In moderately-differentiated tubular adenocarcinoma all three cases also showed polysomies of several chromosomes. The total number of extra chromosomes (polysomy was counted as 5 copies) was higher in the intestinal type (mean 20.9) than in the diffuse type (mean 14.1). Regional lymph node metastasis, vein invasion, or perineural invasion was not related to any specific chromosomal numerical aberration in gastric cancer. Chromosomes X, 1, 2, 3, 4, 15, 17, and 20 had extra copies especially polysomy in most cases. However, chromosomes 7 and 18 revealed monosomy in many cases (31.3% and 33.3% respectively, and chromosome 9 and 11 revealed trisomy in 35.7% and 75% each. Numerically, the most conserved chromosome in gastric cancer was chromosome 12 (62.5%). By flow cytometry, two diploidy and 8 aneuploidy cases with the DNA indices from 1.30 to 1.85 were found.
Adult↗